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    Crenolanib (CP-868596; RO 002; ARO 002)
    Crenolanib (CP-868596; RO 002; ARO 002)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0580
    CAS #: 670220-88-9 Purity ≥98%

    Description: Crenolanib (formerly also known as CP868596; RO-002; ARO-002), a benzimidazole compound, is an orally bioavailable and selective small molecule inhibitor of platelet-derived growth factor receptor (PDGFRα/β) with potential anticancer activity. It inhibits PDGFRα/β with Kd values of 2.1 nM/3.2 nM in CHO cells. Crenolanib is an investigational drug being developed by AROG company in clinical trials for treating various types of cancer, such as acute myeloid leukemia, gastrointestinal stromal tumor, and glioma. Crenolanib acts by binding to and inhibiting PDGFR, which may result in the inhibition of PDGFR-related signal transduction pathways, and, so, the inhibition of tumor angiogenesis and tumor cell proliferation. 

    References: Clin Cancer Res. 2012 Aug 15;18(16):4375-84

    Related CAS: 670220-93-6 (Crenolanib besylate)

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    Molecular Weight (MW)443.54
    CAS No.670220-88-9(free); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 89 mg/mL (200.6 mM)
    Water:<1 mg/mL
    Ethanol: 7 mg/mL (15.8 mM)
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
    SynonymsRO 002; ARO 002, CP-868596; ARO-002; CP 868596; CP868596; ARO002; RO-002; RO002 

    Chemical Name: 1-(2-(5-((3-methyloxetan-3-yl)methoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine.


    InChi Code: InChI=1S/C26H29N5O2/c1-26(14-32-15-26)16-33-20-6-7-22-21(13-20)28-17-31(22)24-8-5-18-3-2-4-23(25(18)29-24)30-11-9-19(27)10-12-30/h2-8,13,17,19H,9-12,14-16,27H2,1H3


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    In Vitro

    In vitro activity: Crenolanib is significantly more potent than imatinib in inhibiting the kinase activity of imatinib-resistant PDGFRα kinases (D842I, D842V, D842Y, D1842-843IM, and deletion I843). Crenolanib is 135-fold more otent than imatinib against D842V in the isogenic model system, with an IC50 of approximately 10 nM. Crenolanib inhibits the kinase activity of the fusion oncogene in EOL-1 cell line, which is derived from a patient with chronic eosinophilic leukemia and expresses the constitutively activated FIP1L1- PDGFRα fusion kinase, with IC50 = 21 nM. Crenolanib also inhibits the proliferation of EOL-1 cells with IC50 = 0.2 pM. Crenolanib inhibits the activation of V561D or D842V-mutant kinases expressed in BaF3 cells with IC50 with 85 nM or 272 nM, respectively. Crenolanib inhibits PDGFRα activation in H1703 non-small cell lung cancer cell line which has 24-fold amplification of the 4q12 region that contains the PDGFRα locus, with IC50 with 26 nM. Crenolanib is an orally bioavailable, highly potent and selective PDGFR TKI. Crenolanib is a benzimidazole compound that has IC50s of 0.9 nM and 1.8 nM for PDGFRA and PDGFRB, respectively.

    Kinase Assay: Chinese hamster ovary (CHO) cells are transiently transfected with mutated or wild type PDGFRα constructs and treated with various concentrations of Crenolanib. Experiments involving recombinant DNA are performed using biosafety level 2 conditions in accordance with guidelines. Protein lysates from cell lines are prepared and subjected to immunoprecipitation using anti-PDGFRα antibodies followed by sequential immunoblotting for PDGFRα. Densitometry is performed to quantify drug effect using Photoshop software, with the level of phosphor- PDGFRα normalized to total protein. Densitometry and proliferation experimental results are analyzed using Calcusyn 2.1 software to mathematically determine the IC50 values. The Wilcoxon Rank Sum Test is used to compare the IC50 values of Crenolanib for a given mutation. 

    Cell Assay: EOL-1 cells are added to 96-well plates at densities of 20, 000 cells/well and incubated with Crenolanib for 72 hours before measuring cellular proliferation using a 2,3-bis[2-methoxyl-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide (XTT)-based assay.

    In VivoCrenolanib (10 mg/kg and 20 mg/kg) suppresses non-small-cell lung cancer tumor growth in vivo and induces tumor cell apoptosis, and the dosage of crenolanib applied is well tolerated by recipient mice.
    Animal modelMice: A549 cells are injected into the axillary regions of mice (2×106 cells/mouse). When the tumor volumes reached 70 mm3, the mice are randomLy allocated to the control group, low-dose crenolanib group (10 mg/kg), or high-dose crenolanib group (20 mg/kg) (n=6 per group). The vehicle for crenolanib treatment consists of 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300. The tumor size and mouse body weight are measured every other day for about 2 weeks. The tumor volume is calculated as follows: (mm3)=(width×width×length)/2. After treatment, the mice are euthanized using carbon dioxide, and the tumors are harvested and analyzed. 
    Formulation & Dosage10, 20 mg/kg; dissolved in 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300
    ReferencesClin Cancer Res. 2012 Aug 15;18(16):4375-84; Onco Targets Ther. 2014 Sep 26;7:1761-8.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Crenolanib (CP-868596)

    Crenolanib (CP-868596)
    Crenolanib (CP-868596)


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